Agomelatine

SKU: orb1308595

Description

Agomelatine (Valdoxan) is a melatonin analog that acts as a melatonin receptor agonist and a 5-HT2C receptor antagonist. It is widely used in neuroscience research, particularly in studies of depression, circadian rhythms, and sleep disorders, utilizing both in vitro binding assays and in vivo behavioral models.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 138112-76-2
• MW: 243.3
• Purity: 99.92% (May vary between batches)
• Formula: C₁₅H₁₇NO₂
• SMILES: COC1=CC=C2C=CC=C(CCNC(C)=O)C2=C1
• Target: 5-HT Receptor,Melatonin Receptor,Endogenous Metabolite
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:42 mg/mL (172.63 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (8.22 mM);DMSO:250 mg/mL (1027.54 mM)

Bioactivity

• Target IC50:
  5-HT2C (human):6.2(pKi)|MT2 (human):0.27 nM (Ki, HEK Cells)|MT2 (human):0.12 nM (Ki, CHO Cells)|5-HT2C (porcine):6.4(pKi)|MT1 (human):0.1 nM (Ki, CHO Cells)|MT1 (human):0.06 nM (Ki, HEK Cells)
• In Vivo:
  In mice subjected to chronic electroshock stress, Agomelatine fully normalized the survival of stress-affected cells in the hippocampus and partially reversed the reduction in glucocorticoid receptor expression.
• In Vitro:
  Agomelatine enhances cell proliferation and neurogenesis in the ventral hippocampus (VH) of adult rats, a region associated with emotional disorders. It effectively reverses behavior alterations in transgenic mice observed in Porsolt forced swimming tests and elevated plus mazes. Agomelatine significantly accelerates the re-adjustment of circadian rhythms of temperature and activity after induced phase shifts. It increases the duration of positive social interactions in mice exposed to new environments. In the ventral dentate gyrus of rats, which is involved in emotional responses, Agomelatine promotes cell proliferation and neurogenesis, consistent with its anti-depressant and anti-anxiety properties. Across the entire dentate gyrus, Agomelatine boosts the survival of newly generated neurons. It enhances the ratio of mature to immature neurons and promotes dendritic sprouting in the granule cells of adult rats, indicating accelerated maturation. Furthermore, Agomelatine activates several cellular signaling pathways (extracellular signal-regulated kinases 1/2, protein kinase B, and glycogen synthase kinase 3 beta) known to be modulated by antidepressants and involved in proliferation/survival control.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Thymanax, Serotonin Receptor, S 20098, S20098, S-20098, Valdoxan, Melatonin Receptor, MelatoninReceptor, inhibit, Inhibitor, MT1, MT2, 5HTReceptor, 5-HT, 5-hydroxytryptamine Receptor, Agonist, Agomelatine, 5-HT2C, 5-HT Receptor, 5HT Receptor, Antagonist, antidepressant, disorder, depressive

Compound Identifiers

PubChem CID

82148